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Assay Detail

CHEMBL638724

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Binding
Binding affinity against adenosine A1 receptor in bovine cortical membranes using [3H]CHA as radioligand
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL4975)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
Ferrarini PL, Betti L, Cavallini T, Giannaccini G, Lucacchini A, Manera C, Martinelli A, Ortore G, Saccomanni G, Tuccinardi T.
J Med Chem (2004) 47 : 3019 -3031
PubMed 15163184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 7.21 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97760 1 9.82
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.60
CHEMBL102429 1 9.25
CHEMBL97687 1 9.15
CHEMBL104998 1 9.00
CHEMBL329294 1 8.80
CHEMBL97757 1 8.39
CHEMBL102430 1 8.28
CHEMBL97895 1 8.28
CHEMBL97549 1 8.28
CHEMBL313864 1 8.28
CHEMBL104999 1 8.17
CHEMBL102178 1 8.14
CHEMBL316630 1 8.00
CHEMBL95384 1 7.96
CHEMBL321769 1 7.82
CHEMBL97037 1 7.80
CHEMBL97337 1 7.77
CHEMBL323303 1 7.64
CHEMBL97896 1 7.58
CHEMBL97624 1 7.55
CHEMBL102753 1 7.32
CHEMBL103150 1 7.32
CHEMBL103559 1 7.30
CHEMBL418797 1 7.16
CHEMBL329293 1 7.10
CHEMBL94538 1 7.00
CHEMBL102491 1 6.80
CHEMBL103588 1 6.68
CHEMBL102974 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97760 Ki = 0.15 nM 9.82
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.25 nM 9.60
CHEMBL102429 Ki = 0.56 nM 9.25
CHEMBL97687 Ki = 0.7 nM 9.15
CHEMBL104998 Ki = 1.0 nM 9.00
CHEMBL329294 Ki = 1.6 nM 8.80
CHEMBL97757 Ki = 4.1 nM 8.39
CHEMBL102430 Ki = 5.3 nM 8.28
CHEMBL97895 Ki = 5.2 nM 8.28
CHEMBL97549 Ki = 5.3 nM 8.28
CHEMBL313864 Ki = 5.3 nM 8.28
CHEMBL104999 Ki = 6.8 nM 8.17
CHEMBL102178 Ki = 7.2 nM 8.14
CHEMBL316630 Ki = 9.9 nM 8.00
CHEMBL95384 Ki = 11.0 nM 7.96
CHEMBL321769 Ki = 15.0 nM 7.82
CHEMBL97037 Ki = 16.0 nM 7.80
CHEMBL97337 Ki = 17.0 nM 7.77
CHEMBL323303 Ki = 23.0 nM 7.64
CHEMBL97896 Ki = 26.0 nM 7.58
CHEMBL97624 Ki = 28.0 nM 7.55
CHEMBL102753 Ki = 48.0 nM 7.32
CHEMBL103150 Ki = 48.0 nM 7.32
CHEMBL103559 Ki = 50.0 nM 7.30
CHEMBL418797 Ki = 70.0 nM 7.16
CHEMBL329293 Ki = 80.0 nM 7.10
CHEMBL94538 Ki = 100.0 nM 7.00
CHEMBL102491 Ki = 160.0 nM 6.80
CHEMBL103588 Ki = 210.0 nM 6.68
CHEMBL102974 Ki = 290.0 nM 6.54
CHEMBL317411 Ki = 340.0 nM 6.47
CHEMBL17127 SCH-58261 Ki = 357.0 nM 6.45
CHEMBL105000 Ki = 380.0 nM 6.42
CHEMBL415697 Ki = 450.0 nM 6.35
CHEMBL97665 Ki = 550.0 nM 6.26
CHEMBL96576 Ki = 810.0 nM 6.09
CHEMBL97778 Ki = 1000.0 nM 6.00
CHEMBL100121 Ki = 1200.0 nM 5.92
CHEMBL98227 Ki = 1300.0 nM 5.89
CHEMBL103796 Ki = 1900.0 nM 5.72
CHEMBL323288 Ki = 4700.0 nM 5.33
CHEMBL328214 Ki = 4900.0 nM 5.31
CHEMBL319580 Ki = 6000.0 nM 5.22
CHEMBL97344 Ki = 6900.0 nM 5.16
CHEMBL103553 Ki = 7000.0 nM 5.16
CHEMBL96617 Ki = 8700.0 nM 5.06
CHEMBL441815 Ki > 10000.0 nM -
CHEMBL321330 Ki > 10000.0 nM -
CHEMBL103278 Ki > 10000.0 nM -
CHEMBL102126 Ki > 10000.0 nM -